Table 3: Development status of antibody agents targeting TLR signaling pathway for SLE treatment.

From: Toll-like receptors: potential targets for lupus treatment

CompoundTargetDescriptionIndicationClinical phaseDosage regimenRef
OPN-305TLR2 antagonistHumanized monoclonal IgG4κ antibody targeting TLR2Myelodysplastic syndrome;
Transplant rejection;
Autoimmune diseases
Phase II1.5 mg/kg, iv (patients, efficacy and safety study)97,98
NI-0101TLR4 antagonistHumanized monoclonal antibody binding to human TLR4Inflammation;
Autoimmune disorders
Phase I≤15 mg/kg, iv (healthy objects, tolerability study)99
Mab 9F3Anti-IFN-αMurine monoclonal antibody that neutralizes human IFN-αType 1 diabetes; SLEBiological testing--
13H5Anti-IFN-αHuman monoclonal IgG1 antibody against human IFN-αTransplant rejection; SLEBiological testing--
ACO-1Anti-IFN-αIgG2a murine monoclonal antibody against IFN-αPsoriasis; SLEBiological testing--
AGS-009 (NNC-0152-0000-0001)Anti-IFN-αHumanized monoclonal IgG4 antibody targeting human IFN-αSLEPhase I0.01-30 mg/kg, iv (patients, tolerability study)105
Rontalizumab (PRO-155767)Anti-IFN-αRecombinant humanized monoclonal antibody targeting human IFN-αSLEPhase II (Discontinued)750 mg, once/4 week, iv or 300 mg, once/2 week, sc (patients, efficacy and safety study)100
Sifalimumab (MEDI-545; MDX-1103)Anti-IFN-αFull human monoclonal IgG1 antibody targeting human IFN-αInflammatory myopathy;
Myositis; Polymyositis;
Psoriasis; SLE
Phase II200, 600 and 1200 mg, once/2 week, iv (patients, efficacy and safety study)101,102,103,104
Anifrolumab (MEDI-546; MDX-1333)Anti-IFN α receptor 1Full human monoclonal IgG1κ antibody targeting the type I IFN receptor 1Scleroderma; SLEPhase II/III100, 300 and 1000 mg, once/4 week, iv (patients, efficacy and safety study)106,107